作者:Hua Zhou、Zhi Sen Wang、Xin Hua Liu、Fei Hu Chen
DOI:10.1016/j.bmc.2018.04.042
日期:2018.7
A series of new 6-styryl-naphthalene-2-amidrazone derivatives were synthesized and evaluated as potential ASIC1a inhibitors. Among them, compound 5e showed the most activity to inhibit [Ca2+]i. elevation in acid-induced articular chondrocytes. Together with the important role of ASIC1a in the pathogenesis of tissue acidification diseases including rheumatoid arthritis, these results might provide a
合成了一系列新的6-苯乙烯基萘-2-氨基dra酮衍生物,并将其评估为潜在的ASIC1a抑制剂。其中,化合物5e显示出抑制[Ca 2+] i的最大活性。酸诱导的关节软骨细胞升高。连同ASIC1a在包括类风湿性关节炎在内的组织酸化疾病的发病机理中的重要作用,这些结果可能为开发针对组织酸化疾病的药物提供有意义的提示或启发。